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    Peficitinib (ASP-015K, JNJ-54781532)
    Peficitinib (ASP-015K, JNJ-54781532)

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    This product is for research use only, not for human use. We do not sell to patients.
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    InvivoChem Cat #: V0321
    CAS #: 944118-01-8 Purity ≥98%

    Description: Peficitinib (formerly ASP015K and JNJ54781532) is a novel, potent and orally bioavailable inhibitor of Janus kinase-JAK with potential anti-inflammatory activities. It inhibits JAK1, JAK2, JAK3 and Tyk2 with IC50 values of 3.9, 5.0, 0.7 and 4.8 nM, respectively. It exhibited potent in vivo anti-rheumatoid arthritis (RA) efficacy in adjuvant-induced arthritis model in rats. In addition, ASP-015K inhibited the IL-2-induced proliferation of human T cells with IC50 of 18 nM.  

    References: Arthritis Rheumatol. 2016 Oct 16. doi: 10.1002/art.39955; Ann Rheum Dis. 2016 Jun;75(6):1057-64.

    Related CAS: 1353219-05-2 (HBr); 944118-01-8 (free base); 

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    Molecular Weight (MW)326.39
    CAS No.944118-01-8 (free base); 
    Storage-20℃ for 3 years in powder form
    -80℃ for 2 years in solvent
    Solubility (In vitro)DMSO: 65 mg/mL (199.1 mM)
    Water: <1 mg/mL
    Ethanol: <1 mg/mL
    Solubility (In vivo)Chemical Name: 4-(((1R,2r,3S,5s,7s)-5-hydroxyadamantan-2-yl)amino)-1H-pyrrolo[2,3-b]pyridine-5-carboxamide
    SMILES Code: O=C(C1=CN=C(NC=C2)C2=C1N[[email protected]]3[[email protected]]4([H])C[[email protected]@]5([H])C[[email protected]](C4)(O)C[[email protected]]3([H])C5)N
    SynonymsJNJ54781532; JNJ54781532; JNJ 54781532; ASP015K; ASP015K; ASP 015K; Peficitinib;

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    In Vitro

    In vitro activity: ASP015K suppresses the IL-2-induced proliferation of human T cells with greater potency than EPO-induced proliferation of human erythroleukemia cells. In human whole blood, ASP015K inhibits STAT5 phosphorylation (pSTAT5).

    Kinase Assay: Human JAK1, JAK2, JAK3, TYK2-domains assays performed using streptavidin-coated 96-well plates. Reaction mixture contained 15 mM Tris-HCl (pH 7.5), 0.01% Tween 20, 2 mM dithiothreitol, 10 mM MgCl2, 250 nM Biotin-Lyn-Substrate-2 (for JAK1, 2 and 3) or Biotin-IRS1-Substrate (for TYK2), and ATP (at final concentrations of 200 μM [JAK1], 10 μM [JAK2], 8 μM [JAK3], and 4 μM [TYK2]). Peficitinib or tofacitinib is dissolved in DMSO. The reaction is initiated by adding the kinase domain, followed by incubation at room temperature for 1 h. Kinase activity is measured as the rate of phosphorylation of Biotin-Lyn-Substrate-2 or Biotin-IRS-Substrate using HRP-conjugated anti-phosphotyrosine antibody (HRP-PY-20) using a phosphotyrosine-specific ELISA. TYK2 kinase assay of Peficitinib is performed with the ATP concentration of 10 μM

    Cell Assay: Erythropoietin regulates haematopoiesis (the production of blood cells). Treatment with ASP015K inhibited the human T-cell proliferation induced by IL-2. And this effect was greater than the effect to inhibit EPO-induced human erythroleukemia cell proliferation. In human whole blood, ASP015K concentration-dependently inhibited STAT5 phosphorylation (pSTAT5). 

    In VivoIn the rat AIA model, ASP015K (p.o.) significantly decreases paw swelling and ankle bone destruction score.
    Animal modelIn healthy volunteers, STAT5-P was dose-dependently inhibited by ASP015K. When the doses of ASP015K were 60, 120, 200, or 300 mg, the mean peak percentage inhibitions of STAT5-P were 84%, 85%, 92%, and 93%, respectively. Plasma ASP015K inhibited STAT5-P with an EC50 value of 48 ng/mL, a shape factor (γ) of ~1.2, and an estimated Emax close to 100%. On days 1, 7, and 14, at ~2 hours after treatment with ASP015K at multiple doses, the peak of median percentage of STAT5-P inhibition appeared.  
    Formulation & DosageFor the oral administration regimen, four of the adjuvant-injected groups receive Peficitinib (1, 3, 10, and 30 mg/kg) dissolved in 0.5% methylcellulose (MC) once daily. Rats in the normal and control groups receive 0.5% MC alone.
    ReferencesArthritis Rheumatol. 2016 Oct 16. doi: 10.1002/art.39955; Ann Rheum Dis. 2016 Jun;75(6):1057-64.

    These protocols are for reference only. InvivoChem does not independently validate these methods.

    Peficitinib (ASP015K, JNJ-54781532)

    American College of Rheumatology (ACR) response rates at week 12 (full analysis set population). Ann Rheum Dis. 2016 Jun;75(6):1057-64.

    Peficitinib (ASP015K, JNJ-54781532)

    Peficitinib (ASP015K, JNJ-54781532)Efficacy variables of mean changes from baseline in the (A) ACR20, (B) DAS28-CRP, (C) HAQ-DI and (D) CRP over time.


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